CA2500498C - Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations - Google Patents

Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations Download PDF

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Publication number
CA2500498C
CA2500498C CA2500498A CA2500498A CA2500498C CA 2500498 C CA2500498 C CA 2500498C CA 2500498 A CA2500498 A CA 2500498A CA 2500498 A CA2500498 A CA 2500498A CA 2500498 C CA2500498 C CA 2500498C
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CA
Canada
Prior art keywords
group
cftr
hydroxyl
nitro
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
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CA2500498A
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English (en)
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CA2500498A1 (fr
Inventor
Alan Verkman
Tonghui Ma
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University of California
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University of California
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Priority claimed from US10/262,573 external-priority patent/US20040063695A1/en
Application filed by University of California filed Critical University of California
Publication of CA2500498A1 publication Critical patent/CA2500498A1/fr
Application granted granted Critical
Publication of CA2500498C publication Critical patent/CA2500498C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system

Abstract

L'invention concerne des compositions, des préparations pharmaceutiques et des procédés permettant d'inhiber la protéine CFTR, utiles pour l'étude et le traitement des maladies dont la médiation est assurée par la protéine CFTR. Les compositions et les préparations pharmaceutiques peuvent comprendre un ou plusieurs composés thiazolidinone, et par ailleurs un ou plusieurs vecteurs, excipients et/ou adjuvants pharmaceutiquement acceptables. Les procédés consistent, selon certaines variantes, à administrer au patient soufrant d'une maladie ou d'une affection dont la médiation est assurée par la protéine CFTR une quantité efficace de composé thiazolidinone. Sous d'autres variantes, on décrit des procédés inhibant la protéine CFTR qui consistent à mettre en contact des cellules du patient avec une quantité efficace de composé thiazolidinone. L'invention concerne également un modèle animal non humain de maladie dont la médiation est assurée par la protéine CFTR, résultant de l'administration d'un composé thiazolidinone à un animal non humain, en quantité suffisante pour inhiber la protéine CFTR.
CA2500498A 2002-09-30 2003-09-30 Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations Expired - Fee Related CA2500498C (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US10/262,573 2002-09-30
US10/262,573 US20040063695A1 (en) 2002-09-30 2002-09-30 Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof
US48025303P 2003-06-20 2003-06-20
US60/480,253 2003-06-20
PCT/US2003/031005 WO2004028480A2 (fr) 2002-09-30 2003-09-30 Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations

Publications (2)

Publication Number Publication Date
CA2500498A1 CA2500498A1 (fr) 2004-04-08
CA2500498C true CA2500498C (fr) 2012-08-21

Family

ID=32044981

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2500498A Expired - Fee Related CA2500498C (fr) 2002-09-30 2003-09-30 Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations

Country Status (13)

Country Link
EP (1) EP1549321A4 (fr)
JP (1) JP4977319B2 (fr)
KR (1) KR20050061501A (fr)
CN (1) CN100356922C (fr)
AP (1) AP2005003292A0 (fr)
AU (1) AU2003277162C1 (fr)
BR (1) BR0314943A (fr)
CA (1) CA2500498C (fr)
EA (1) EA009847B1 (fr)
MX (1) MXPA05003366A (fr)
NZ (1) NZ538809A (fr)
PL (1) PL376147A1 (fr)
WO (1) WO2004028480A2 (fr)

Cited By (1)

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US8796321B2 (en) 2008-04-21 2014-08-05 Path Drug Solutions Compounds, compositions and methods comprising oxadiazole derivatives

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US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
HUE055205T2 (hu) 2006-04-07 2021-11-29 Vertex Pharma ATP-kötõ kazetta transzporterek modulátorainak elõállítása
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
CN101668732A (zh) 2007-04-02 2010-03-10 同一世界健康研究院 Cftr抑制剂化合物及其用途
ES2578735T3 (es) * 2007-08-24 2016-07-29 Vertex Pharmaceuticals Incorporated Isotiazolopiridinonas útiles para el tratamiento de (entre otros) fibrosis quística
US8507524B2 (en) 2007-11-16 2013-08-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette-transporters
US8507534B2 (en) 2007-12-07 2013-08-13 Vertex Pharmaceuticals Incorporated Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
EP2279029A2 (fr) * 2008-03-25 2011-02-02 The Regents of the University of California Inhibiteurs à petite molécule soluble dans l eau du régulateur de conductance transmembranaire de fibrose kystique
US8227615B2 (en) 2008-03-31 2012-07-24 Vertex Pharmaceutical Incorporated Pyridyl derivatives as CFTR modulators
US8236838B2 (en) 2008-04-21 2012-08-07 Institute For Oneworld Health Compounds, compositions and methods comprising isoxazole derivatives
US20110237528A1 (en) * 2008-09-19 2011-09-29 Institute For Oneworld Health Compositions and methods comprising imidazole and triazole derivatives
US8343976B2 (en) 2009-04-20 2013-01-01 Institute For Oneworld Health Compounds, compositions and methods comprising pyrazole derivatives
EP2490696A1 (fr) * 2009-10-20 2012-08-29 INSERM (Institut National de la Santé et de la Recherche Médicale) Méthodes et compositions pharmaceutiques pour le traitement des troubles de l'homéostasie du glucose
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
RU2711481C2 (ru) 2010-03-25 2020-01-17 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДЫЕ ФОРМЫ (R)-1-(2, 2-ДИФТОРБЕНЗО[d][1, 3]ДИОКСОЛ-5-ИЛ)-N-(1-(2, 3-ДИГИДРОКСИПРОПИЛ)-6-ФТОР-2-(1-ГИДРОКСИ-2-МЕТИЛПРОПАН-2-ИЛ)-1H-ИНДОЛ-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДА
AR081069A1 (es) 2010-04-07 2012-06-06 Vertex Pharma Formas solidas del acido 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoico
JP2013523833A (ja) 2010-04-07 2013-06-17 バーテックス ファーマシューティカルズ インコーポレイテッド ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の医薬組成物およびその投与
CA2797118C (fr) 2010-04-22 2021-03-30 Vertex Pharmaceuticals Incorporated Procede de production de composes de cycloalkylcarboxamido-indole
US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
US20120046330A1 (en) 2010-08-23 2012-02-23 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (r)-1-(2,2-difluorobenzo[d] [1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration thereof
CN102133402B (zh) * 2011-03-24 2013-06-12 首都医科大学附属北京同仁医院 囊性纤维化跨膜转导调节因子抑制剂在制备治疗糖尿病药物中的应用
JP6014816B2 (ja) 2011-05-10 2016-10-26 国立大学法人神戸大学 Ｒａｓ機能阻害作用を有するチオキソチアゾリジン誘導体
EP2776427B1 (fr) 2011-11-08 2017-02-01 Vertex Pharmaceuticals Incorporated Modulateurs de transporteurs de cassette de liaison à l'atp
CA3128556A1 (fr) 2012-01-25 2013-08-01 Vertex Pharmaceuticals Incorporated Formulations d'acide 3-(6-(1-(2,2-difluorobenzo [d] [1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoique
EP2872122A1 (fr) 2012-07-16 2015-05-20 Vertex Pharmaceuticals Incorporated Compositions pharmaceutiques de (r)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide et son administration
SG10201703452PA (en) 2012-11-02 2017-06-29 Vertex Pharma Pharmaceutical compositions for the treatment of cftr mediated diseases
FR2999191B1 (fr) 2012-12-12 2016-02-05 Lesaffre & Cie Souches probiotiques pour le traitement et/ou la prevention de la diarrhee
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PL3203840T3 (pl) 2014-10-06 2021-01-11 Vertex Pharmaceuticals Incorporated Modulatory mukowiscydozowego przezbłonowego regulatora przewodnictwa
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Also Published As

Publication number Publication date
CN100356922C (zh) 2007-12-26
AP2005003292A0 (en) 2005-06-30
WO2004028480A3 (fr) 2004-07-01
EP1549321A4 (fr) 2007-05-23
EP1549321A2 (fr) 2005-07-06
JP2006503853A (ja) 2006-02-02
MXPA05003366A (es) 2005-10-05
BR0314943A (pt) 2005-08-02
PL376147A1 (en) 2005-12-27
EA009847B1 (ru) 2008-04-28
AU2003277162C1 (en) 2009-12-24
AU2003277162B2 (en) 2009-07-16
CN1684686A (zh) 2005-10-19
JP4977319B2 (ja) 2012-07-18
KR20050061501A (ko) 2005-06-22
WO2004028480A2 (fr) 2004-04-08
NZ538809A (en) 2008-06-30
CA2500498A1 (fr) 2004-04-08
EA200500583A1 (ru) 2005-12-29
AU2003277162A1 (en) 2004-04-19

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